Abstract：
:In order to prepare fine granules of sparfloxacin (SPFX), a new quinolone anti-bacterial drug that shows masking of the bitter taste of SPFX and dissolutes at a rapid rate, various film-coated fine granules containing 20% SPFX and 0-52% low-substituted hydroxypropylcellulose(L-HPC) in the cores, were prepared by a spray method. Mixtures of ethylcellulose (EC), hydroxypropylmethylcellulose (HPMC), titanium dioxide and sucrose stearate in weight ratios of X:Y:2:1 (X + Y = 6) were used as film materials. The degree of masking of the bitter taste by water-insoluble film, mainly consisting of EC and HPMC, increased by increasing the content ratio of EC to HPMC and the amount of films, but was also slightly affected by the amount of L-HPC in the cores, which were coated with either EC or EC/HPMC (4/2). On the other hand, the dissolution rate increased with an increased amount of L-HPC in the cores and with a decreasing ratio of EC to HPMC in the films. Increasing the amount of L-HPC in the cores, which induced a considerable expansion of the fine granules owing to their taking up of water from the dissolution medium, resulted in bursting of the film after a short lag time. The bioavailability of the film-coated fine granules containing 20% SPFX and 52% L-HPC in the cores and 10% EC/HPMC (4/2) in the coating film, which masked the bitter taste of SPFX and showed the optimal release characteristics, was equivalent to that of conventional tablets containing 100 mg SPFX in beagle dogs.
journal_name
Biol Pharm Bulljournal_title
Biological & pharmaceutical bulletinauthors
Shirai Y,Sogo K,Yamamoto K,Kojima K,Fujioka H,Makita H,Nakamura Ydoi
10.1248/bpb.16.172subject
Has Abstractpub_date
1993-02-01 00:00:00pages
172-7issue
2eissn
0918-6158issn
1347-5215journal_volume
16pub_type
杂志文章abstract：:Alpha1-adrenoceptor antagonists are clinically useful for the improvement of urinary obstruction due to benign prostatic hyperplasia (BPH), and their therapeutic effects are mediated through the blockade of prostatic alpha(1)-adrenoceptors. The present study was undertaken to predict the magnitude and duration of alph...
journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/bpb.30.1237
更新日期：2007-07-01 00:00:00
abstract：:There may be cardio-renal interactions in rats of isoproterenol-induced heart failure, which may be associated with renal fibrosis and endothelial-to-mesenchymal transition (EndMT). Since its discovery, relaxin (RLX) which was regarded as a reproductive hormone for a long time, is recently considered an effective anti...
journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/bpb.b16-00882
更新日期：2017-01-01 00:00:00
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journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/bpb.31.99
更新日期：2008-01-01 00:00:00
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journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章,评审
doi：10.1248/bpb.b16-00867
更新日期：2017-01-01 00:00:00
abstract：:Phospholipase (PL) A2 activity prepared from isolated rat fat pads incubated with sodium orthovanadate (vanadate) was increased in a time- and dose-dependent manner. The increasing effect of vanadate was reduced in the presence of tyrosine kinase inhibitors. Under the inhibition of protein synthesis by cycloheximide, ...
journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/bpb.18.347
更新日期：1995-02-01 00:00:00
abstract：:The gastric mucus is an important factor in the gastric mucosal protection from acid, pepsin and various reagents (alcohol, aspirin, etc.). MUC5AC is the mucin secreted from surface mucous cells, and belongs to the gel-forming mucin. We examined the regulation of rat MUC5AC (rMUC5AC) mRNA by glucocorticoid in vivo and...
journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/bpb.24.634
更新日期：2001-06-01 00:00:00
abstract：:A protein was purified from rabbit seminal plasma using preparative acrylamide disc electrophoresis, ammonium sulfate precipitation and gel filtration. The protein inhibited the in vitro fertilization of mouse ova inseminated with epididymal sperm and with capacitated sperm. The inhibition was not observed, however, w...
journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/bpb.16.453
更新日期：1993-05-01 00:00:00
abstract：:A fungus of Pestalotiopsis species produced an extracellular, water-soluble polysaccharide (PS-N). PS-N exhibited significant hypoglycemic activity in streptozotocin-induced diabetic mice following intraperitoneal administration and had an effect on oral glucose tolerance in normal mice following oral administration. ...
journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/bpb.20.118
更新日期：1997-02-01 00:00:00
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journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/bpb.29.211
更新日期：2006-02-01 00:00:00
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journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/bpb.22.873
更新日期：1999-08-01 00:00:00
abstract：:Alzheimer's beta-amyloid protein (A beta) is the main component of senile plaques, which are characteristic hallmarks of the Alzheimer's disease brain. Recently, there have been several reports that A beta has toxic effects on both cultured neurons and in the brain. We confirmed the neurotoxicity of A beta in vitro an...
journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/bpb.18.1750
更新日期：1995-12-01 00:00:00
abstract：:The first-pass intestinal metabolism of 5-fluorouracil (5-FU) was investigated by single-pass perfusion of the rat small intestine. At the low concentration of 0.06 mg/ml, the fraction of 5-FU absorbed into (i.e., appeared in) the mesenteric venous blood (Fa,b) was about 50% smaller than the fraction absorbed (disappe...
journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/bpb.21.871
更新日期：1998-08-01 00:00:00
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journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/bpb.b12-00228
更新日期：2012-01-01 00:00:00
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journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/bpb.b20-00350
更新日期：2020-08-01 00:00:00
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journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/bpb.27.404
更新日期：2004-03-01 00:00:00
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journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/bpb.32.755
更新日期：2009-04-01 00:00:00
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journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/bpb.26.1170
更新日期：2003-08-01 00:00:00
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journal_title：Biological & pharmaceutical bulletin
pub_type： 临床试验,杂志文章
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更新日期：2014-01-01 00:00:00
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journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章
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journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/bpb.28.260
更新日期：2005-02-01 00:00:00
abstract：:Indomethacin is used as an anti-inflammatory drug and a nonselective cyclooxygenase inhibitor. When indomethacin in methanol was photo-irradiated with an Hg lamp, methyl ester, ethyl ester, and gamma-lactone derivatives of indomethacin were produced. In the present study, we found that the methyl ester derivative of i...
journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/bpb.28.2206
更新日期：2005-12-01 00:00:00
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journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/bpb.32.427
更新日期：2009-03-01 00:00:00
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journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/bpb.16.982
更新日期：1993-10-01 00:00:00
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journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/bpb.21.823
更新日期：1998-08-01 00:00:00
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journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/bpb.33.316
更新日期：2010-01-01 00:00:00
abstract：:Ginsenosides, the unique constituents and secondary metabolites of the Panax species, have been known to be the pharmacologically active ingredients of ginseng. Recently, our research group has developed a new processed ginseng, called Sun ginseng (SG), which has an increased amount of the red ginseng unique ginsenosi...
journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/bpb.29.2051
更新日期：2006-10-01 00:00:00
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journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/bpb.b14-00099
更新日期：2014-01-01 00:00:00
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journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/bpb.35.796
更新日期：2012-01-01 00:00:00
abstract：:The effects of ketoconazole (KCZ) on secretion of progesterone and cAMP in Leydig cells were investigated in vitro. MA-10 mouse Leydig tumor cells were used to conduct the experiments. KCZ significantly inhibited the progesterone production from MA-10 cells in a dose dependent fashion between 2 and 20 microM among 1, ...
journal_title：Biological & pharmaceutical bulletin
pub_type： 杂志文章
doi：10.1248/bpb.25.794
更新日期：2002-06-01 00:00:00
